发明授权
- 专利标题: Peptidylaminodiols
- 专利标题(中): 肽基氨基二醇
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申请号: US217106申请日: 1988-07-11
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公开(公告)号: US4845079A公开(公告)日: 1989-07-04
- 发明人: Jay R. Luly , Jacob J. Plattner , Dale J. Kempf
- 申请人: Jay R. Luly , Jacob J. Plattner , Dale J. Kempf
- 专利权人: Luly Jay R,Plattner Jacob J,Kempf Dale J
- 当前专利权人: Luly Jay R,Plattner Jacob J,Kempf Dale J
- 主分类号: A61K38/00
- IPC分类号: A61K38/00 ; C07D233/54 ; C07K5/02 ; C07K5/06 ; C07K5/065 ; C07K5/078 ; C07K5/08 ; C07K5/083 ; C07K5/097
摘要:
A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is C.dbd.O or CHOH; U is CH.sub.2 or NR.sub.2, provided that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-napththyl)methyl, (4-imidazoyl)methyl, .alpha.,.alpha.-dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, loweralkenyl, benzyl or heterocyclic ring substituted methyl; R.sub.4 is loweralkyl, cycloalkylmethyl or benzyl; R.sub.5 is vinyl, formyl, hydroxymethyl or hydrogen; R.sub.7 is hydrogen or loweralkyl; R.sub.8 and R.sub.9 are independently selected from OH and NH.sub.2 ; and R.sub.6 is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R.sub.5 and R.sub.7 are both hydrogen and R.sub.8 and R.sub.9 are OH, the carbon bearing R.sub.5 is of the "R" configuration and the carbon bearing R.sub.6 is of the "S" configuration; or pharmaceutically acceptable salts or esters thereof. Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.
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